GABAB Receptors

Supporting information

GABAB receptors are metabotropic G-protein-coupled receptors responsible for mediating the inhibitory effects of GABA alongside ionotropic GABAA and GABAA-ρ receptors. They exist as heterodimers of GABAB1 and GABAB2 subunits and the presence of both subunits is required for receptor function.

When GABAB1 is expressed alone it is non-functional and is not transported to the cell membrane. This subunit is responsible for binding GABA, and the GABAB2 subunit interacts with the G protein. The two subunits interact allosterically: GABAB1 increases coupling of GABAB2 to G proteins and GABAB2 increases agonist binding to GABAB1. GABAB receptors are coupled to Ca2+ and K+ channels.

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